New methods for the synthesis of biologically active phenanthridine-based libraries
dc.contributor.advisor
Hulme, Alison N.
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dc.contributor.advisor
Lam, Hon Wai
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dc.contributor.author
Donaldson, Lauren Rona
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dc.date.accessioned
2012-01-18T10:40:38Z
dc.date.available
2012-01-18T10:40:38Z
dc.date.issued
2009-06-29
dc.description.abstract
Small molecule libraries have become essential for the development of drug
discovery campaigns and chemical genetics. The studies towards the synthesis of a
small molecule library, based upon the cis-ring fused phenanthridine core I, will be
described. The first section of this thesis examines the development and application of a novel
intramolecular Heck cyclisation to the synthesis of core phenanthridine structure II,
via precursor III (Chapter 2).The second section (Chapter 3) describes the extension of this methodology towards
the development of a library of phenanthridines IV. This includes methodology
designed to incorporate the key principles of diversity-oriented synthesis, namely
appendage, stereochemical and skeletal diversity. The final part of this thesis (Chapter 4) describes the merging of these various
methodologies to generate a small library of novel phenanthridine analogues.
Preliminary biological evaluation of the phenanthridine library using whole organism
zebrafish phenotyping, will also be discussed.
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dc.identifier.uri
http://hdl.handle.net/1842/5736
dc.language.iso
en
dc.publisher
The University of Edinburgh
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dc.relation.hasversion
Donaldson, L. R; Haigh, D.; Hulme, A. N. Tetrahedron 2008, 64, 4468-4477.
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dc.subject
small molecule library
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dc.subject
phenanthridine
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dc.subject
intramolecular Heck cyclisation
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dc.title
New methods for the synthesis of biologically active phenanthridine-based libraries
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dc.type
Thesis or Dissertation
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dc.type.qualificationlevel
Doctoral
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dc.type.qualificationname
PhD Doctor of Philosophy
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